drugs related to balance
DESCRIPTION
DRUGS RELATED TO BALANCE. BALANCE. BALANCE. BALANCE. BALANCE. BALANCE. DRUGS RELATED TO BALANCE. ILOs:. BALANCE. Recognize causes and symptoms of balance disorders. Identify the transmitters involved in vestibular transmission - PowerPoint PPT PresentationTRANSCRIPT
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BALANCEBALANCE
BALANCE
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BALANCEBALANCE
BALANCE
Recognize causes and symptoms of balance disorders.
Identify the transmitters involved in vestibular transmission
Segregate classes of drugs used in the management protocols to control or prevent vertigoIdentify drugs that can precipitate vertigo
ILOs:
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Fluid in the semi-circular canal [in plane of the movement] lags→ stimulating nerve endings → firing impulses along the vestibular nerve
To vestibular nuclei → relay stations
+ +++ ++
++ +
+
Impulses come also from eyes, touch and position sensors in the neck, spine and limbs
The processed output goes
Conscious brain interpreted as a sense of position in space
Eye muscles to stabilize
Neck spine & limbs to control posture and movement
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COMPENSATING / STABILIZING MOVEMENTS
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TRANSMITTERS INVOLVED IN VESTIBULAR FIRING
Main TransmittersGlutamatesAcetylcholineGlycineGABA
Modulatory Transmitters HistamineNoradrenaline
++++++++
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The individual will feel unsteady when standing or walking
When disorder sets in = BALANCE DISORDER
DIZZINESS ?
VERTIGO?
Lighted headedness
It is a type of dizziness that creates the sense
That you or your environment is SPINNING
Sensation of disorientation or motion (spinning) + – Nausea or vomiting,– sweating, – abnormal eye movements (nystagmus)
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CAUSES CNS
Inner ear
Others
Vestibular hair cell stimulation unrelated to head and body motions
Impact on vestibular nuclei , afferent inputs or efferent outputs
Fluid / Electrolyte / Ca disturbances; ↑ BP, ↑ cholesteroldiabetes, anemia , calcium disorders …..
Low tolerance for vehicular motion such as cars, boats, cruise ships, and airplanes that cause MOTION SICKNESS.
↓ equalization of air pressure in middle ear due to blocking or swelling of Eustachian tube → undue pressure on inner ear
MENIERE’S
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PATHOPHYSIOLOGY
Perilymph
Endolymph
Inner ear chamber is filled with perilymph & endolymph.
↑endolymphatic pressure ( hydrolymphatic hydrops )→ microscopice breaks of separating membrane often with vestibular hair loss → depolarization and functional loss
Ménière's disease; disorder of control of inner ear fluid homeostasis
Ménière's disease is a disorder of the inner ear that can affect hearing and balance.It is characterized by episodes of vertigo, tinnitus and progressive hearing loss .
Inner ear
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Drugs used to control or prevent vertigo episodes
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THERAPEUTIC MANAGEMENT
Intend to dull brain response
to vestibular signals from inner ear
Intend to suppress acute attacks [ tame vertigo episodes]
Vestibular Suppressants
Prevent Recurrence
Diuretics (but not loop diuretics)
Corticosteroids L-type Ca Channel Blockers
( fluid retention )(inflammation)
cinnarazine, flunnarazine, verapamilNB. If migraine is also present → add on its treatment
+ EmesisSpinning ( vasodilatation )
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VESTIBULAR SUPRESSANTS
Antihistamine Anticholinergic
ANTIEMETICS
Emesis
H1 antagonistMeclizineDimenhydrinate
Prochlorperazine Promethazine
+Dopamine antagonists + Sedation
MetoclopramideDomperidone NO cross BBB
Dopamine Antagonist +Gastroprokinetic
Dopamine Antagonists
Phenothiazines
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VESTIBULAR SUPRESSANTS
LorazepamClonazepam Diazepam
promote & facilitate central vestibular compensation via GABA modulation
Benzodiazepines
H1 agonists Betahistine ???H3 antagonists
Spinning
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H 2
H 1
H 3
H istamine
Mediator
NeurotransmitterCNSANS
H 3
+
+
+
H 1
-ve presynaptic autoregulation
Betahistine
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BETAHISTINE
Weak agonist at H1 receptors → regulates inner ear fluid homeostasis (labyrinthine circulation ) → inducing vaso-dilatation in middle ear → relieves pressure in inner earStrong antagonism of H3 autoreceptors → ↑ augmenting effects on H1 receptors in the brain →
- ↑ H synthesis in tuberomammillary nuclei of the posterior hypothalamus to promote & facilitate central vestibular compensation
- ↑ H release in vestibular nuclei ↑levels of neurotransmitters such as 5HT in the brainstem, which inhibits the activity of vestibular nuclei.
H1 agonists
H3 antagonists
VESTIBULAR SUPRESSANTS
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BETAHISTINE
PharmacokineticsTablet form , rapidly & completely absorbedt½=2-3hPartially metabolized ( active) & excreted in urine
ADRsHeadacheNauseaGastric effects↓ appetite and weight loss
Contraindications
Peptic ulcerPheochromocytomaBronchial asthma
VESTIBULAR SUPRESSANTS
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DIMENHYDRINATE (Dramamine ) H1 antagonistAntihistamines
> antiemetic < sedating than Meclizine
Block H1 receptors in CRTZSedative effectsWeak anticholinergic effects
In vertigoIn control of MOTION SICKNESS by ↓ excitability in the labyrinth & blocking conduction in vestibular-cerebellar pathways.
ADRsSedationDizzinessAnticholinergic side effects
ContraindicationsGlaucoma Prostatic enlargement
Indications
ANTIEMETICS
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PROCHlORPERAZINEBlock dopamine receptors at CRTZ Antipsychotic , some sedation + antiemetic
Indications One of the best antiemetics in vertigo (sedating & has some vestibular suppressant action)
Dopamine Antagonists
A Piperazine Phenothiazines
METOCLOPRAMIDEA potent central antiemetic acting on CRTZ Has some sedating action Has potent gastroprokinetic effect
Restlessness or drowsiness Extrapyramidal manifestations on prolonged use
ADRs
ANTIEMETICS
IndicationsIn vertigo
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DRUGS INDUCING VERTIGO
Are those drugs (or chemicals) producing destructive damaging effects on structure or function of labyrinthine hair cells &/ or their neuronal connections
FUNCTIONAL
VESTIBULOTOXINS
Drugs altering fluid & electrolyte Diuretics
Antihypertensives ….Drugs altering vestibular firing
Anticonvulsants Antidepressants Sedative hypnotics Alcohol Cocaine
MIXED OTOTOXINS
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DRUGS INDUCING VERTIGO
Aminoglycoside antibiotics; gentamycin, kanamycin, neomycin, streptomycin, tobramycin, netlimycin Fluroquinolines, Vancomycin, PolymixinQuinine, chloroquine, quinidineNitrogen mustardLoop diureticsNSAIDsTobacco
MIXED OTOTOXINS
FUNCTIONAL
STRUCTURAL
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DRUGS INDUCING VERTIGO
Aminoglycoside antibiotics; streptomycin, kanamycin, neomycin, gentamycin, tobramycin, netlimycin
Neomycin → activate caspases → Death Receptor PathwayGentamycin → evoke free radicals
→ Mitochondrial Pathway
Apoptosis
STRUCTURAL
Quinine, chloroquine, quinidineLoop diureticsNSAIDs
↓local blood flow → biochemical changes → alter electromechanical transduction
Firing of impulses
FUNCTIONAL
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GOODLUCK